AU731267B2 - Mesylate dihydrate salts of 5-(2-(4-(1,2-benzis othiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2 (1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist - Google Patents

Mesylate dihydrate salts of 5-(2-(4-(1,2-benzis othiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2 (1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist Download PDF

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Publication number
AU731267B2
AU731267B2 AU21747/97A AU2174797A AU731267B2 AU 731267 B2 AU731267 B2 AU 731267B2 AU 21747/97 A AU21747/97 A AU 21747/97A AU 2174797 A AU2174797 A AU 2174797A AU 731267 B2 AU731267 B2 AU 731267B2
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AU
Australia
Prior art keywords
compound
disorder
composition
chloro
schizophrenia
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Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
AU21747/97A
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English (en)
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AU2174797A (en
Inventor
Frank Robert Busch
Carol Anne Rose
Russell James Shine
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Pfizer Inc
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Pfizer Inc
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Application granted granted Critical
Publication of AU731267B2 publication Critical patent/AU731267B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
AU21747/97A 1996-05-07 1997-04-10 Mesylate dihydrate salts of 5-(2-(4-(1,2-benzis othiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2 (1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist Ceased AU731267B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US1675796P 1996-05-07 1996-05-07
US60/016757 1996-05-07
PCT/IB1997/000393 WO1997042191A1 (en) 1996-05-07 1997-04-10 Mesylate dihydrate salts of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2(1h)-indol-2-one (=ziprasidone), its preparation and its use as dopamine d2 antagonist

Publications (2)

Publication Number Publication Date
AU2174797A AU2174797A (en) 1997-11-26
AU731267B2 true AU731267B2 (en) 2001-03-29

Family

ID=21778804

Family Applications (1)

Application Number Title Priority Date Filing Date
AU21747/97A Ceased AU731267B2 (en) 1996-05-07 1997-04-10 Mesylate dihydrate salts of 5-(2-(4-(1,2-benzis othiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2 (1H)-indol-2-one (=ziprasidone), its preparation and its use as dopamine D2 antagonist

Country Status (41)

Country Link
US (1) US6245765B1 (he)
EP (1) EP0918772B1 (he)
JP (1) JP3494659B2 (he)
KR (1) KR100333215B1 (he)
CN (1) CN1091769C (he)
AP (1) AP765A (he)
AR (1) AR007004A1 (he)
AT (1) ATE278689T1 (he)
AU (1) AU731267B2 (he)
BG (1) BG63544B1 (he)
BR (1) BR9709889A (he)
CA (1) CA2252898C (he)
CO (1) CO4940466A1 (he)
CZ (1) CZ289215B6 (he)
DE (1) DE69731094T2 (he)
DK (1) DK0918772T3 (he)
DZ (1) DZ2222A1 (he)
EA (1) EA001190B1 (he)
EG (1) EG24076A (he)
ES (1) ES2229342T3 (he)
GT (1) GT199700052A (he)
HK (1) HK1017892A1 (he)
HR (1) HRP970236B1 (he)
ID (1) ID16867A (he)
IL (1) IL126591A (he)
IS (1) IS2080B (he)
MA (1) MA24171A1 (he)
MY (1) MY119997A (he)
NO (1) NO312514B1 (he)
NZ (1) NZ332218A (he)
OA (1) OA10909A (he)
PL (1) PL188330B1 (he)
PT (1) PT918772E (he)
SI (1) SI0918772T1 (he)
SK (1) SK282837B6 (he)
TN (1) TNSN97074A1 (he)
TR (1) TR199802240T2 (he)
TW (1) TW491847B (he)
UA (1) UA46840C2 (he)
WO (1) WO1997042191A1 (he)
ZA (1) ZA973876B (he)

Families Citing this family (28)

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HN1996000101A (es) * 1996-02-28 1997-06-26 Inc Pfizer Terapia combinada para la osteoporosis
UA57734C2 (uk) 1996-05-07 2003-07-15 Пфайзер Інк. Комплекси включення арилгетероциклічних солей
IL127497A (he) * 1997-12-18 2002-07-25 Pfizer Prod Inc תכשירים רפואיים המכילים תרכובות פיפראזיניל-הטרוציקליות לטיפול בהפרעות פסיכיאטריות
US20080113025A1 (en) * 1998-11-02 2008-05-15 Elan Pharma International Limited Compositions comprising nanoparticulate naproxen and controlled release hydrocodone
EE200200670A (et) * 2000-06-02 2004-08-16 Pfizer Products Inc. S-metüüldihüdroziprasidoon psühhiaatriliste ja silmahaiguste raviks
US20040048876A1 (en) * 2002-02-20 2004-03-11 Pfizer Inc. Ziprasidone composition and synthetic controls
UY27668A1 (es) 2002-02-20 2003-10-31 Pfizer Prod Inc Composición de ziprasidona y controles sintéticos
CA2525366A1 (en) * 2003-05-16 2004-11-25 Pfizer Products Inc. Therapeutic combinations of atypical antipsychotics with gaba modulators, anticonvulsants or benzodiazapines
US20050043324A1 (en) * 2003-06-03 2005-02-24 Tamas Koltai Polymorphic forms of ziprasidone HCI and processes for their preparation
WO2005040160A2 (en) 2003-10-24 2005-05-06 Teva Pharmaceutical Industries Ltd. Processes for preparation of ziprasidone
MXPA06013163A (es) * 2004-05-11 2007-02-13 Pfizer Prod Inc Combinacion de antipsicoticos atipicos y antagonistas del receptor 5-ht1b.
CA2467538C (en) 2004-05-14 2010-08-24 Apotex Pharmachem Inc. New amorphous ziprasidone hydrochloride (5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2h-indol-2-one hydrochloride) and processes to produce the same
CA2471219A1 (en) 2004-06-14 2005-12-14 Apotex Pharmachem Inc. Improved preparation of an anhydrate form of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2h-indol-2-one hydrochloride (ziprasidone hydrochloride)
US7777037B2 (en) * 2004-10-27 2010-08-17 Dr. Reddy's Laboratories Limited Ziprasidone process
EP2623095A1 (en) * 2004-11-16 2013-08-07 Elan Pharma International Limited Injectable nanoparticulate olanzapine formulations
WO2006086787A1 (en) * 2005-02-11 2006-08-17 Teva Pharmaceutical Industries Ltd. Process of preparing ziprasidone mesylate
EP1863806A1 (en) * 2005-02-11 2007-12-12 Teva Pharmaceutical Industries Ltd Amorphous ziprasidone mesylate
EP1855651A4 (en) * 2005-03-03 2011-06-15 Elan Pharma Int Ltd NANOPARTICULAR COMPOSITIONS OF HETEROCYCLIC AMIDE DERIVATIVES
ITMI20050346A1 (it) 2005-03-07 2006-09-08 Dipharma Spa Forma solida di ziprasidone cloridrato
CA2500667C (en) 2005-03-11 2013-01-15 Apotex Pharmachem Inc. Preparation of acid addition salts of ziprasidone and intermediates thereof by solid phase-gas phase reactions
EP1858891A2 (en) * 2005-03-14 2007-11-28 Teva Pharmaceutical Industries Ltd. Crystalline forms of ziprasidone mesylate
WO2006099452A1 (en) * 2005-03-14 2006-09-21 Teva Pharmaceutical Industries Ltd. Anhydrous ziprasidone mesylate and a process for its preparation
ITMI20052216A1 (it) * 2005-11-18 2007-05-19 Dipharma Spa Procedimento per la preparazione di ziprasidone
CA2683276A1 (en) * 2007-05-18 2008-11-27 Scidose Llc Ziprasidone formulations
WO2009156889A1 (en) * 2008-06-25 2009-12-30 Pfizer Inc. Diaryl compounds and uses thereof
WO2012053654A1 (en) * 2010-10-18 2012-04-26 Dainippon Sumitomo Pharma Co., Ltd. Sustained-release formulation for injection
SI23610A (sl) 2011-01-13 2012-07-31 Diagen@d@o@o Nove adicijske soli ziprasidona postopek za njihovo pripravo in njihova uporaba v terapiji
JP6440625B2 (ja) 2012-11-14 2018-12-19 ザ・ジョンズ・ホプキンス・ユニバーシティー 精神***病を処置するための方法および組成物

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0584903A1 (en) * 1992-08-26 1994-03-02 Pfizer Inc. Process for preparing aryl piperazinyl-heterocyclic compounds

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX173362B (es) * 1987-03-02 1994-02-23 Pfizer Compuestos de piperazinil heterociclicos y procedimiento para su preparacion
US4831031A (en) * 1988-01-22 1989-05-16 Pfizer Inc. Aryl piperazinyl-(C2 or C4) alkylene heterocyclic compounds having neuroleptic activity
US5312925A (en) * 1992-09-01 1994-05-17 Pfizer Inc. Monohydrate of 5-(2-(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one-hydrochloride
US5359068A (en) * 1993-06-28 1994-10-25 Pfizer Inc. Processes and intermediates for the preparation of 5-[2-(4-(benzoisothiazol-3-yl)-piperazin-1-yl)ethyl]-6-chloro-1,3-dihydro-indol-2-one
JP3102896B2 (ja) 1996-05-07 2000-10-23 ファイザー インク． ５―（２―（４―（１，２―ベンズイソチアゾール―３―イル）―１―ピペラジニル）エチル）―６―クロロ―１，３―ジヒドロ―２（１ｈ）―インドール―２―オン（＝ジプラシドン）のメシレート三水和物、その調製法およびドーパミンｄ２アンタゴニストとしてのその使用

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0584903A1 (en) * 1992-08-26 1994-03-02 Pfizer Inc. Process for preparing aryl piperazinyl-heterocyclic compounds

Also Published As

Publication number Publication date
UA46840C2 (uk) 2002-06-17
AR007004A1 (es) 1999-10-13
DK0918772T3 (da) 2005-01-10
ES2229342T3 (es) 2005-04-16
MA24171A1 (fr) 1997-12-31
PT918772E (pt) 2004-12-31
EP0918772B1 (en) 2004-10-06
DE69731094T2 (de) 2006-02-23
CA2252898C (en) 2003-04-08
PL329884A1 (en) 1999-04-12
KR100333215B1 (ko) 2002-06-20
NO985194L (no) 1998-11-06
DZ2222A1 (fr) 2002-12-03
EA001190B1 (ru) 2000-12-25
CA2252898A1 (en) 1997-11-13
AP9700976A0 (en) 1997-07-31
EG24076A (en) 2008-05-11
OA10909A (en) 2001-10-26
ID16867A (id) 1997-11-20
KR20000010824A (ko) 2000-02-25
TW491847B (en) 2002-06-21
BG102892A (en) 1999-09-30
CZ289215B6 (cs) 2001-12-12
EA199800912A1 (ru) 1999-04-29
SK150898A3 (en) 2000-02-14
WO1997042191A1 (en) 1997-11-13
DE69731094D1 (de) 2004-11-11
CZ349398A3 (cs) 1999-09-15
ATE278689T1 (de) 2004-10-15
HRP970236A2 (en) 1998-06-30
IL126591A (he) 2001-11-25
BG63544B1 (bg) 2002-04-30
CN1216991A (zh) 1999-05-19
AU2174797A (en) 1997-11-26
CN1091769C (zh) 2002-10-02
IL126591A0 (en) 1999-08-17
NO985194D0 (no) 1998-11-06
JPH11509867A (ja) 1999-08-31
JP3494659B2 (ja) 2004-02-09
IS4874A (is) 1998-10-20
AP765A (en) 1999-09-17
BR9709889A (pt) 1999-08-10
NO312514B1 (no) 2002-05-21
TR199802240T2 (he) 1999-02-22
TNSN97074A1 (fr) 2005-03-15
ZA973876B (en) 1998-11-06
US6245765B1 (en) 2001-06-12
EP0918772A1 (en) 1999-06-02
GT199700052A (es) 2001-08-29
MY119997A (en) 2005-08-30
HK1017892A1 (en) 1999-12-03
PL188330B1 (pl) 2005-01-31
HRP970236B1 (en) 2002-12-31
CO4940466A1 (es) 2000-07-24
IS2080B (is) 2006-02-15
SI0918772T1 (en) 2005-02-28
NZ332218A (en) 2005-02-25
SK282837B6 (sk) 2002-12-03

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